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Tranexamic Acid

INCI Name

:

Tranexamic acid

Synonyms

:

m-tranexamic acid

Chemical Name

:

trans-4-(aminomethyl)cyclohexanecarboxylic acid

CAS No.

:

701-54-2

EINECS No.

:

214-818-2

Molecular Formula

:

C8H15NO2

Molecular Weight

:

157.2

Chemical Class

:

Amino acids

Main Functions

:

Whitening agent; Skin roughness improving agent

Structure:

 

Typical Specification

Appearance

:

A white crystalline powder

Solubility

:

Freely soluble in water and in glacial acetic acid, practically insoluble in alcohol and in acetone

pH

:

7.0-8.0

Related substance

 

 

Impurity A

:

≤ 0.1%

Impurity B

:

≤ 0.2%

Any other impurity

:

≤ 0.1%

All other Impurities

:

≤ 0.2%

Bromic

:

Not more than 670ppm

Assay

:

99.0-101.0%

Functions

1

Whitening and prevent pigmentation

 

•    

Reduce or remove the pigmentation of skin

 

 

Prevent and/or treat pigmentations such as chloasmas, freckles, sunburn, dark skin and melanoderma caused by a drug such as steroid

 

•    

Minimize dark spot area due to sun exposure.

 

•    

Anti-inflammation

 

 

Act on the chronic mild inflammatory condition at the sites of spots, to suppress melanocyte activation

2

Inhibit or improve skin roughness

 

Restore damaged skin caused by UVA/UVB, pollution or other environmental factors.

Mechanism of whitening skin

•    

Block melanin formation path induced by ultraviolet rays

•    

Prevent melanin accumulation

•    

Decreases melanocyte tyrosinase activity by preventing the binding of plasminogen to the keratinocytes, which results in reduction of prostaglandins and arachidonic acid, which are inflammatory mediators involved in melanogenesis.

Synergistic effects with other whitening ingredients

Tranexamic acid produces good synergistic effect when combined with ascorbic acid or its derivatives such as magnesium ascorbyl phosphate, 3-O-ethyl ascorbic acid, disodium adenosine triphophate, escinol (deacylated product of escin under hydrolysis by sodium methylate), L-cysteine. Penetration enhancers helps the transdermic absorption of tranexamic acid into spots.

Application

Tranexamic acid is suitable to all kinds of skin for removing pigmentation, whitening skin and reducing spots, such as:

•    

Pigmentation after sun exposure

•    

Dark spots

•    

Sensitive skin

•    

Acne and inflammation

•    

Postoperative care after laser, pulsed light treatment

 

Efficacy and Safety Comparison of Tranexamic Acid with Other Whitening Ingredients

Tranexamic acid is relatively stable to light, temperature, pH, and oxygen, and no special protections are required to maintain its whitening effect, as compared with conventional whitening ingredients. It is no irritant and no sensitive to skin and is safe for use in whitening cosmetics.

 

Azelaic acid

L- ascorbic acid

arbutin

Tranexaminc acid

Reduction of melanin

 

Inhibit tyrosinase

 

No irritation

 

 

 

Hypoallergenic

 

 

 

Anti-inflammatory

 

 

Use Level: 0.5% ( cosmetics); cosmaceuticals: 2.0-3.0%

[BACKGROUND]

1.    Route of Melanin Formation

In melanocyte

:

It is generally thought that biosynthesis of melanin occurs in a cytoplasmic granule, melanosome, in the melanocyte via a complex pathway in which tyrosine is oxidized by tyrosinase to cause biosynthesis of dopa and dopaquinone, and the dopaquinone is converted into indolequinone or the like due to auto-oxidation by ultraviolet rays.

Outside of melanocyte

:

It has become clear that melanin, which so far has been considered to be formed only in melanocytes, is also formed outside of melanocytes.

It was found that the quick skin darkening under the sun is due to the colorless pre-melanin DHICA (precursor of melanin) which has accumulate in the epidermis is converted to melanin upon exposure to ultraviolet A rays (long wave length).

When transparent DHICA solution was irradiated with UVA equivalent to about 20 minutes of exposure to sunlight in the summer, pre-melanin was converted to melanin in a short time.

Melanin and inflammation

:

At the sites where spots develop, excessive melanin formation constantly takes place. It was found that inflammatory cells are more abundant at the site of the spot than at the normal site (the inflammation at the spot site is extremely slight and does not manifest as redness, swelling or pain). It was also discovered that the number of activated melanocytes (melanin-producing cells) to total melanocytes is higher at the spot site than at the normal site. From these results, we may assume that melanocytes remain activated because of "a chronic, mild inflammatory condition" and excessive melanin formation thus persists at the site of the spot.

 

2.   Pigmentations & melasma

Pigmentations such as chloasmas (or melasma), freckles, sunburn, dark skin and melanoderma caused by a drug such as steroid are generated by excess deposition of melanin pigment in the skin.

Melasma is an acquired symmetric hyperpigmentation characterized by irregular light- to gray-brown macules, especially on the face of women.

 

3.        Accidental discovery of whitening effect by tranexamic acid

Tranexamic acid is an antifibrinolytic agent and is used to control excess bleeding. The skin whitening effects of tranexamic acid was occasionally found when it was used as a coagulant to treat aneurismal subarachnoid hemorrhage. And from then on, it was used in physician's prescription to treat liver spots and pigmentation.

The most famous example is that tranexamic acid has been widely used in Shiseido’s whitening series products such as NAVISION IP Essence (TA), NAVISION TA Lotion, NAVISION TA Essence and Melanoreduce EX

 

4.        Clinical Uses of Tranexamic Acid

Bleeding and skin diseases

:

TA has been used clinically for over 30 years to treat abnormal bleeding, as well as skin diseases such as eczema, hives, drug-induced irritation, and toxicodermia, via internal administration, and also orally to treat itching, swelling, and erythema. It is a representative ω-amino aci-type anti-plasmin agent that has a highly specific action on the fibrinolytic system, blocking the conversion of plasminogen to plasmin by inhibiting PA action through the formation of a reversible complex with plasminogen. TA is also thought to form a reversible complex with plasmin, inhibiting the reaction with fibrin.

Pigmentation

:

Kondou et al. have published results from a clinical study examining the effects of a tranexamic acid (TA) emulsion applied topically to melasma and freckles. The study involved 33 subjects, 25 with melasma and 8 with freckles, who applied the TA emulsion for five to eighteen weeks, after which their skin pigmentation was visually assessed by a dermatologist.

Researchers found that the TA emulsion had improved the pigmentation in 20 subjects with melasma (80%) and 6 subjects (75%) with freckles. No side effect was recognized and thus the TA emulsion was deemed safe. In regard to changes over the course of the study, marked improvement was observed within eight weeks for melasma but within 12 weeks for freckles; therefore, improvement was considered to require at least two months of topical application. The authors concluded the TA emulsion was an effective cosmeceutical that provided a whitening effect on melasma and freckles through inhibition of melanin synthesis. It also prevented the appearance of new pigment spots and freckles.

Melasma

:

In an open pilot study, intradermal microinjection of tranexamic acid was given to 100 women with melasma for 12 weeks. The treatment was well tolerated, and 76.5% of the subjects reported fair lightening of their melasma.

Documentation:
Formulation



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